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1
Relative beta-lactamase- and transpeptidase-inhibitory activities of the new quinolone WIN-57273 in Staphylococcus aureus.新型喹诺酮WIN-57273对金黄色葡萄球菌的相对β-内酰胺酶和转肽酶抑制活性
Antimicrob Agents Chemother. 1992 Apr;36(4):894-7. doi: 10.1128/AAC.36.4.894.
2
Antibacterial activity of a new tetracyclic quinolone, No. 5290, against norfloxacin- and ciprofloxacin-resistant strains of Staphylococcus aureus.新型四环喹诺酮类药物5290对耐诺氟沙星和环丙沙星金黄色葡萄球菌菌株的抗菌活性
Chem Pharm Bull (Tokyo). 1991 Oct;39(10):2644-6. doi: 10.1248/cpb.39.2644.
3
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Antimicrob Agents Chemother. 1990 Jun;34(6):1123-7. doi: 10.1128/AAC.34.6.1123.
4
Comparative in vitro activities of a new quinolone, WIN 57273, and piperacillin plus tazobactam against anaerobic bacteria.新型喹诺酮类药物WIN 57273与哌拉西林加他唑巴坦对厌氧菌的体外比较活性
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Effect of hydrophobicity and molecular mass on the accumulation of fluoroquinolones by Staphylococcus aureus.疏水性和分子量对金黄色葡萄球菌积累氟喹诺酮类药物的影响。
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Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus.新型氟喹诺酮类药物加替沙星（AM - 1155、CG5501、BMS - 206584）对金黄色葡萄球菌序贯获得性喹诺酮耐药突变株及norA转化株的抗菌活性。
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Activity of BMS-284756, a novel des-fluoro(6) quinolone, against Staphylococcus aureus, including contributions of mutations to quinolone resistance.新型去氟（6）喹诺酮类药物BMS-284756对金黄色葡萄球菌的活性，包括喹诺酮耐药性突变的作用。
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引用本文的文献

1
Quinolone mode of action--new aspects.喹诺酮类药物的作用模式——新的方面。
Drugs. 1993;45 Suppl 3:8-14. doi: 10.2165/00003495-199300453-00004.

本文引用的文献

1
Membrane-bound penicillinases in Gram-positive bacteria.革兰氏阳性菌中的膜结合青霉素酶。
J Biol Chem. 1982 Apr 25;257(8):4490-5.
2
The beta-lactamases of gram-negative bacteria and their possible physiological role.革兰氏阴性菌的β-内酰胺酶及其可能的生理作用。
Adv Microb Physiol. 1973;9:31-88. doi: 10.1016/s0065-2911(08)60376-8.
3
Regulation of penicillin-binding protein activity: description of a methicillin-inducible penicillin-binding protein in Staphylococcus aureus.青霉素结合蛋白活性的调节：金黄色葡萄球菌中一种甲氧西林诱导型青霉素结合蛋白的描述。
Antimicrob Agents Chemother. 1985 May;27(5):828-31. doi: 10.1128/AAC.27.5.828.
4
Contribution of beta-lactamase hydrolysis and outer membrane permeability to ceftriaxone resistance in Enterobacter cloacae.β-内酰胺酶水解和外膜通透性对阴沟肠杆菌头孢曲松耐药性的作用
Antimicrob Agents Chemother. 1987 Oct;31(10):1589-95. doi: 10.1128/AAC.31.10.1589.
5
Evolution of an inducible penicillin-target protein in methicillin-resistant Staphylococcus aureus by gene fusion.通过基因融合在耐甲氧西林金黄色葡萄球菌中诱导型青霉素靶蛋白的进化
FEBS Lett. 1987 Aug 31;221(1):167-71. doi: 10.1016/0014-5793(87)80373-3.
6
Characterization of an isogenic set of methicillin-resistant and susceptible mutants of Staphylococcus aureus.金黄色葡萄球菌耐甲氧西林和敏感突变体同基因集的表征
Eur J Clin Microbiol. 1986 Dec;5(6):697-701. doi: 10.1007/BF02013308.
7
Methicillin resistance in Staphylococcus epidermidis. Relationship between the additional penicillin-binding protein and an attachment transpeptidase.表皮葡萄球菌中的耐甲氧西林特性。额外青霉素结合蛋白与附着转肽酶之间的关系。
Eur J Biochem. 1989 Oct 20;185(1):211-8. doi: 10.1111/j.1432-1033.1989.tb15104.x.
8
Differentiation of beta-lactamase variants of Staphylococcus aureus by substrate hydrolysis profiles.通过底物水解谱区分金黄色葡萄球菌的β-内酰胺酶变体
J Infect Dis. 1989 Jan;159(1):103-8. doi: 10.1093/infdis/159.1.103.
9
Synergistic effect of quinolones and oxacillin on methicillin-resistant Staphylococcus species.喹诺酮类药物与苯唑西林对耐甲氧西林葡萄球菌属的协同作用。
Antimicrob Agents Chemother. 1989 Dec;33(12):2037-41. doi: 10.1128/AAC.33.12.2037.
10
In vitro evaluation of WIN 57273, a new broad-spectrum fluoroquinolone.新型广谱氟喹诺酮类药物WIN 57273的体外评价
Antimicrob Agents Chemother. 1990 Feb;34(2):306-13. doi: 10.1128/AAC.34.2.306.

新型喹诺酮WIN-57273对金黄色葡萄球菌的相对β-内酰胺酶和转肽酶抑制活性

Relative beta-lactamase- and transpeptidase-inhibitory activities of the new quinolone WIN-57273 in Staphylococcus aureus.

作者信息

Furet Y X, Lucain C, Pechère J C

机构信息

Département de Microbiologie Médicale, Centre Médical Universitaire, Geneva, Switzerland.

出版信息

Antimicrob Agents Chemother. 1992 Apr;36(4):894-7. doi: 10.1128/AAC.36.4.894.

DOI:10.1128/AAC.36.4.894
PMID:1323958
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC189483/
Abstract

The new quinolone WIN-57273 was shown to inhibit Staphylococcus aureus beta-lactamase activity noncompetitively in vitro with an apparent Ki value of 0.5 mM. MICs of penicillin G for a highly quinolone-resistant, beta-lactamase-negative strain in the presence of exogenous beta-lactamase decreased considerably when subinhibitory concentrations of WIN-57273 were added. Furthermore, the attachment transpeptidase reaction, investigated on whole cells of S. aureus, was impeded by WIN-57273 concentrations of greater than or equal to 30 microM. While these interactions suggest a novel mechanism of action for this compound, they are probably not relevant to the overall antibacterial potency of WIN-57273.

摘要

新型喹诺酮WIN-57273在体外被证明能以非竞争性方式抑制金黄色葡萄球菌β-内酰胺酶活性，其表观抑制常数（Ki）值为0.5 mM。当添加亚抑制浓度的WIN-57273时，在存在外源性β-内酰胺酶的情况下，青霉素G对高度耐喹诺酮、β-内酰胺酶阴性菌株的最低抑菌浓度（MIC）显著降低。此外，在金黄色葡萄球菌全细胞上研究的转肽酶连接反应，在WIN-57273浓度大于或等于30 microM时受到阻碍。虽然这些相互作用表明该化合物有新的作用机制，但它们可能与WIN-57273的整体抗菌效力无关。